Fluconazole

Description overdue on 28.11.2011

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Antifungal drug. It provides highly specific action that inhibits the enzyme activity of fungi, which are dependent on P450 . The mechanism of action is based on blocking the transition lanosterol   at ergosterol   fungal cells, breaks replication Growth and increases the permeability of cell membranes. Fluconazole not affect the enzymes in the human body, it acts selectively only against fungi, unlike clotrimazole, itraconazole . ketoconazole   econazole and that affect microsomal oxidation   in the liver. Fluconazole has no antiadrogennogo action. Highly effective against Opportunistic fungal infections . It is produced in the form of capsules, solution, powder, syrup, in tablet form.

Indications:

Fluconazole prescribed for systemic lesions Cryptococcus fungi   (sepsis, meningitis ) disseminated candidiasis , Generalized candidemia, mucosal candidiasis ( candiduria , Bronchopulmonary, invasive candidiasis, atrophic candidiasis ). The drug is effective for genital candidiasis: balanitis, acute and recurrent course vaginal candidiasis . Fluconazole is used for deep, endemic mycoses ( histoplasmosis, sporotrichosis, koktsidiodoz ), Cutaneous mycosis   ( chromophytosis . onychomycosis , The defeat of the body, feet, groin).

Contraindications:

Fluconazole is not indicated in case of hypersensitivity to azole antifungals, failure renal and hepatic systems, pregnancy, alcoholism, breast-feeding. Not applicable in Pediatrics (6 months).

Side effect:

Forming Organs : petechiae , Bleeding, thrombocytopenia, leukopenia, agranulocytosis, neutropenia. Nervous system : Convulsions, dizziness, headache, fatigue. Digestive system : Dyspepsia, flatulence , Epigastric pain, violation of stool, loss of appetite. Allergic reactions : Stevens-Johnson syndrome . erythema multiforme exudative , Anaphylactic shock. Other reactions: alopecia, hypokalemia, disruption of the renal system, hypertriglyceridemia . hypercholesterolemia . In case of overdose observed paranoid behavior . hallucinations . Requires gastric lavage, holding forced diuresis , Hemodialysis.

Mode of application:

Disseminated candidiasis kindidemii, cryptococcal infection Invasive Candida infections: the first day - 400 mg on subsequent days at 200-400 mg once a day. The duration of therapy is determined individually depending on disease severity, dynamics. Patients with AIDS and related cryptococcal meningitis   The recommended dosage is 200 mg / day. Oropharyngeal candidiasis   - 50-100 mg per day for a week. Candidiasis of the mucous membranes   treated for months of daily administration of 100 mg per day. Vaginal candidiasis, balanitis   (vyzv. Candida) requires a single injection of 150 mg. Fungal skin lesions   treat this month: 150 mg 1 time in 7 days. Chromophytosis   - 300 mg 2 times at intervals of 7 days. Onychomycosis   - 150 mg every 7 days until a complete change of the nail plate.

Special instructions:

It takes a long, uninterrupted treatment until persistent clinical remission. If premature termination of therapy increases the risk of relapse. Treatment can begin when there is no laboratory test results sowing. During treatment requires monitoring of the liver, kidneys, blood. As necessary, a correction fungicidal treatment . Hepatotoxic effects of the drug on the liver Fluconazole is reversible. With simultaneous use of coumarin anticoagulants is recommended regular monitoring prothrombin index .

Drug Interactions:

Fluconazole increases efficiency coumarin anticoagulants   (warfarin by 12%). The drug increases the spillover effect and increases the concentration of zidovudine, rifabutin   (possible uveitis ), Cyclosporine, phenytoin. Fluconazole increases the half-life theophylline Until intoxication. Simultaneous treatment with sulfonylureas requires regular monitoring of blood sugar levels. Cisapride and terfenadine   can lead to arrhythmias, paroxysms of ventricular tachycardia . Hydrochlorothiazide increases drug level in blood by 40%.